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品質等級
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 10 mg/mL, clear
儲存溫度
−20°C
InChI
1S/C20H24O4/c1-12(2)17-9-15(5-6-19(17)21)10-18-13(3)7-16(8-14(18)4)24-11-20(22)23/h5-9,12,21H,10-11H2,1-4H3,(H,22,23)
InChI 密鑰
QNAZTOHXCZPOSA-UHFFFAOYSA-N
生化／生理作用
Sobetirome也称为2-(4-(4-苄氧基)-3-异丙基苄基)-3,5-二甲基苯氧基)乙酸/GC-1。它在生理pH下具有一个内环和带负电荷的羧酸盐基团。Sobetirome被认为可以降低人体的胆固醇水平。
Sobetirome是甲状腺激素受体（TR） β 和 TRα 的口服活性、强效激动剂，表现出选择性的组织作用。Sobetirome对心脏、骨骼和骨骼肌的无甲状腺毒性作用。
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
Sobetirome prodrug esters with enhanced blood?brain barrier permeability.
Placzek AT, et al.
Bioorganic & Medicinal Chemistry, 24(22), 5842-5854 (2016)
Jan Lammel Lindemann et al.
Expert opinion on therapeutic targets, 20(2), 145-149 (2015-11-14)
Sobetirome binds selectively to the main hepatic form of thyroid hormone (TH) receptor, TRβ1, compared to TRα1, which is principally responsible for thyrotoxic effects on heart, muscle and bone. Sobetirome also preferentially accumulates in liver. It was originally envisaged that
K Kannisto et al.
Atherosclerosis, 237(2), 544-554 (2014-12-03)
Thyroid hormone reduces plasma cholesterol and increases expression of low-density lipoprotein receptor (LDL-R) in liver, an effect mediated by thyroid receptor β (TRβ). The selective TRβ modulator GC-1 also enhances several steps in reverse cholesterol transport and can decrease serum
Ester-to-amide rearrangement of ethanolamine-derived prodrugs of sobetirome with increased blood-brain barrier penetration.
Ferrara SJ, et al.
Bioorganic & Medicinal Chemistry, 25(10), 2743-2753 (2017)
Andrew T Placzek et al.
Bioorganic & medicinal chemistry, 24(22), 5842-5854 (2016-10-26)
There is currently great interest in developing drugs that stimulate myelin repair for use in demyelinating diseases such as multiple sclerosis. Thyroid hormone plays a key role in stimulating myelination during development and also controls the expression of important genes
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